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PubMed Journal Database | Journal of drug targeting RSS

09:42 EDT 24th April 2014 | BioPortfolio

The US National Library of Medicine and National Institutes of Health manage which comprises of more than 21 million records, papers, reports for biomedical literature, including MEDLINE, life science and medical journals, articles, reviews, reports and  books.  BioPortfolio aims to publish relevant information on published papers, clinical trials and news associated with users selected topics.

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Showing PubMed Articles 1–25 of 119 from Journal of drug targeting


Magnetic Catechin-Dextran conjugate as targeted therapeutic for pancreatic tumour cells.

Abstract Background: Catechin-dextran conjugates have recently attracted a lot of attention due to their anticancer activity against a range of cancer cells. Magnetic nanoparticles have the ability to concentrate therapeutically important drugs due to their magnetic-spatial control and provide opportunities for targeted drug delivery. Purpose: Enhancement of the anticancer efficiency of catechin-dextran conjugate by functionalisation with magnetic iron oxide nanoparticles. Methods: Modification of the coati...


Targeted liposomal drug delivery systems for the treatment of B cell malignancies.

Abstract Nanoparticulate systems have demonstrated significant potential for overcoming the limitations of non-specific adverse effects related to chemotherapy. The treatment of blood malignancies employing targeted particulate drug delivery systems presents unique challenges and considerable research has been focused towards the development of targeted liposomal formulations for B cell malignancies. These formulations are aimed at achieving selectivity towards the malignant cells by targeting several cell...


Requisites for successful theranostics with radionuclide-based reporter gene imaging.

Abstract Radionuclide-based theranostic strategy has been widely used in diagnosis and treatment of patients with hyperthyroidism or differentiated thyroid cancer for a long time, and sodium iodide symporter gene is the radionuclide-based reporter gene used in theranostics. Theranostics, which is a promising approach, offering the ideal combination of accurate diagnosis and successful therapy in various clinical fields, is expected to become a key area of personalized medicine. Rapid advancements in biotech...


Inhalable microspheres embedding chitosan-coated PLGA nanoparticles for 2-methoxyestradiol.

Abstract Developing a highly effective and lung-targeted local drug delivery carrier with low irritancy may be critical for improving treatment of lung cancer. Using soluble excipients as microspheres (MS) matrix, respirable MS embedding chitosan-coated poly(d,l-lactide-co-glycolide) nanoparticles (CNP-MS) for 2-methoxyestradiol (2-ME) were designed, which could avoid macrophage phagocytosis to achieve the targeted delivery of these drugs. 2-ME CNP-MS were prepared by spray-drying and characterized by morph...


Liposomes co-modified with cholesterol anchored cleavable PEG and octaarginines for tumor targeted drug delivery.

Abstract Tumor targeted drug delivery system with high efficiency of tumor accumulation, cell internalization and endosomal escape was considered ideal for cancer therapy. Herein, a cleavable polyethylene glycol (PEG) and octaarginines (R8) co-modified liposome (CL-R8-LP) was developed, in which the cholesterol was used as an alternative anchor to the commonest phospholipids for the diversified development of surface modification. The in vitro hemolysis assay and bio-distribution study demonstrated that CL-...


Neonatal Fc receptor (FcRn): a novel target for therapeutic antibodies and antibody engineering.

Abstract The biomedical applications of antibodies as prophylactics, therapeutics and diagnostics are developing rapidly. Neonatal Fc receptor (FcRn) is a major IgG Fc receptor capable of facilitating the translocation of IgG. FcRn can protect IgG from intracellular catabolism, thereby increasing its half-life. In recent decade, the interaction between FcRn and the Fc region has been reported with the focuses on either prolonging the plasma half-life of therapeutic IgG or shortening the half-life of pathoge...


Intranasal therapeutic strategies for management of Alzheimer's disease.

Abstract Alzheimer's disease (AD) is a chronic and progressive age-related irreversible neurodegenerative disorder that represents 70% of all dementia with 35 million cases worldwide. Successful treatment strategies for AD have so far been limited, and present therapy is based on cholinergic replacement therapy and inhibiting glutamate excitotoxicity. In this context, role of neuroprotective drugs has generated considerable interest in management of AD. Recently, direct intranasal (IN) delivery of drug moie...


Development of dual responsive nanocomposite for simultaneous delivery of anticancer drugs.

Abstract In this paper novel stimuli-responsive cationic mesoporous silica nanoparticles (MSNs) were fabricated through the facile polymerization method. The synthesis process was characterized and validated by Fourier transform infrared spectroscopy and hydrogen nuclear magnetic resonance spectroscopy. The prepared nanoparticles were characterized using scanning electron microscopy (SEM), Zeta potential and thermogravimetric analysis methods. SEM results revealed the uniformity in size and shape of nanopar...


Galactosylated poly(ethylene glycol) methacrylate-st-3-guanidinopropyl methacrylamide copolymers as siRNA carriers for inhibiting Survivin expression in vitro and in vivo.

Abstract In this report, galactosylated poly(ethylene glycol) methacrylate-st-3-guanidinopropyl methacrylamide copolymers (galactosylated PEGMA-st-GPMA, GGP) are developed as siRNA carriers to inhibit Survivin mRNA expression. GGPs are combined with Survivin siRNAs to form siRNA/GGP polyplexes. The polyplexes particles were examined by a dynamic light scattering. It showed that GGP copolymers could condense siRNA to form particles with diameter from 128 to 423 nm and zeta potential value in the range from...


Experiments and synthesis of bone-targeting epirubicin with the water-soluble macromolecular drug delivery systems of oxidized-dextran.

Abstract Epirubicin (EPI) is a broad spectrum antineoplastic drug, commonly used as a chemotherapy method to treat osteosarcoma. However, its application has been limited by many side-effects. Therefore, targeted drug delivery to bone has been the aim of current anti-bone-tumor drug studies. Due to the exceptional affinity of Bisphosphonates (BP) to bone, 1-amino-ethylene-1, 1-dephosphate acid (AEDP) was chosen as the bone targeting moiety for water-soluble macromolecular drug delivery systems of oxidized-d...


PirB is a novel potential therapeutic target for enhancing axonal regeneration and synaptic plasticity following CNS injury in mammals.

Abstract A major barrier to axonal regeneration in mammals is the unfavorable extracellular environment that develops following injury to the central nervous system (CNS). In particular, three myelin-associated inhibitory proteins (MAIs) - Nogo, myelin-associated glycoprotein (MAG) and oligodendrocyte myelin glycoprotein (OMgp) - are known to inhibit axonal regeneration and functional recovery. These MAIs share a common receptor, glycosylphosphatidylinositol-anchored Nogo receptor (NgR). However, paired imm...


Evaluation of (131)I-Pentamidine for scintigraphy of experimentally Leishmania tropica infected hamsters.

Abstract We aimed to assess the ability of (131)I-Pentamidine scintigraphy to detect the lesions of Leishmania tropica infection. An experimental model of cutaneous leishmaniasis was developed. The presence of cutaneous leishmaniasis was confirmed. Pentamidine was radioiodinated with (131)I. The radiolabeled pentamidine was validated by the requisite quality control tests to check its radiolabeling efficiency, in vitro stability. (131)I-Pentamidine (activity: 18.5 MBq/100 µl) was injected intracardiaca...


Liposomes formulated with fMLP-modified cholesterol for enhancing drug concentration at inflammatory sites.

Abstract Improving efficacy of inflammation treatment by increasing drug delivery to the inflammatory sites is a challenging endeavor. N-formyl-methionyl-leucyl-phenylalanine (fMLP), the first discovered leukocyte chemotaxis peptide, is composed of formyl methionine, leucine and phenylalanine. It conjugates with formyl peptide receptors on the target cells with high receptor expression on the surface such as macrophages. With this in mind, we developed a novel fMLP-modified liposome (fMLP-LIP) for enhancing...


Improvement of colonic healing by preoperative oral partially hydrolyzed guar gum (Benefiber) in rats which underwent preoperative radiotherapy.

Abstract Background: Neoadjuvant radiotherapy in rectal cancer could interfere with anastomotic healing. We investigated the effects of preoperative oral administration of Benefiber on the healing irradiated colonic anastomosis. Methods: Forty male Wistar rats were divided into four groups. Group I (control group), Group II (Benefiber® pretreatment group), Group III (preoperative radiotherapy group) and Group IV (preoperative radiotherapy and Benefiber® pretreatment group). All animals underwent 1 cm le...


Factors affecting the selectivity of nanoparticle-based photoinduced damage in free and xenografted chorioallantoïc membrane model.

Abstract Background: Photodynamic therapy (PDT) is a minimally invasive treatment modality for selective destruction of tumours. Critical anatomical structures, like blood vessels in close proximity to the tumour, could be harmed during PDT. Purpose: This study aims to discriminate the photoinduced response of normal and cancerous tissues to photodamage induced by liposomal formulations of meta-tetra(hydroxyphenyl)chlorin (mTHPC). Methods: Normal vascular and cancerous tissues were represented, respectively...


Combined delivery of BCNU and VEGF siRNA using amphiphilic peptides for glioblastoma.

Abstract Combined delivery of chemical drug and therapeutic gene has been introduced as an efficient method for the treatment of cancers such as glioblastoma. In this study, bis-chloroethylnitrosourea (BCNU) and vascular endothelial growth factor (VEGF) small interfering RNA (VEGF-siRNA) were co-delivered into C6 glioblastoma cells using a non-toxic peptide-based carrier. The R3V6 peptides, which are composed of 3-arginine and 6-valine, formed self-assembled micelles in aqueous solution. BCNU, a hydrophobic...


Potential use of the complex of doxorubicin with folate-conjugated methyl-β-cyclodextrin for tumor-selective cancer chemotherapy.

Abstract In a recent study, we attempted to confer a tumor-selective cytotoxic activity to methyl-β-cyclodextrin (M-β-CyD), we synthesized folate-conjugated M-β-CyD (FA-M-β-CyD), and demonstrated the potential of FA-M-β-CyD as a novel anticancer agent at a high dose. In the present study, to expand the application of FA-M-β-CyD for cancer chemotherapy, we evaluated the potential of FA-M-β-CyD as a tumor-targeting anticancer drug carrier at a low dose. FA-M-β-CyD formed an inclusion complex with doxo...


Characterization of oleanolic acid derivative for colon cancer targeting with positron emission tomography.

Abstract Oleanolic acid (OA) is a pentacyclic triterpenoid found in various plant species. Triterpenoid compounds have been shown to inhibit tumor proliferation and to induce apoptosis in cancer cells. We synthesized an OA derivative and evaluated its inhibitory effects on cell proliferation in human colon cancer. Radioisotope-labeled OA was prepared for noninvasive monitoring of tumor progression in vitro and in vivo. The OA derivative decreased cell survival in a concentration-dependent manner and increas...


Subcellular drug targeting, pharmacokinetics and bioavailability.

Abstract Effective treatment of diseases at the molecular level is possible by directing the drug substance (micromolecular, protein or peptide drugs, DNA, oligonucleotides, siRNA) with the aid of a specialized nanoparticulate carrier, for safe and effective transport to the specific site of action in the cytosol and its organelles including nuclear targeting. To achieve efficient cytosolic delivery of therapeutics or nuclear targeting, different drug delivery systems (DDS) have been developed (macromolecul...


Brain delivery of proteins via their fatty acid and block copolymer modifications.

Abstract It is well known that hydrophobic small molecules penetrate cell membranes better than hydrophilic molecules. Amphiphilic molecules that dissolve both in lipid and aqueous phases are best suited for membrane transport. Transport of biomacromolecules across physiological barriers, e.g. the blood-brain barrier, is greatly complicated by the unique structure and function of such barriers. Two decades ago we adopted a simple philosophy that to increase protein delivery to the brain one needs to modify...


Spacer length impacts the efficacy of targeted docetaxel conjugates in prostate-specific membrane antigen expressing prostate cancer.

Abstract Combination of targeted delivery and controlled release is a powerful technique for cancer treatment. In this paper, we describe the design, synthesis, structure validation and biological properties of targeted and non-targeted N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-docetaxel conjugates. Docetaxel (DTX) was conjugated to HPMA copolymer via a tetrapeptide spacer (-GFLG-). 3-(1,3-dicarboxypropyl)-ureido]pentanedioic acid (DUPA) was used as the targeting moiety to actively deliver DTX for...


Aptamer-nanoparticle bioconjugates enhance intracellular delivery of vinorelbine to breast cancer cells.

Abstract Targeted uptake of therapeutic nanoparticles in cell- or tissue-specific manner is an attractive technology since they can offer greater efficacy and reduce cytotoxicity on peripheral healthy tissues. In this study, AS1411 (AP), a DNA aptamer specifically binding to nucleolin that is overexpressed on the plasma membrane of breast cancer (BC) cells, was exploited as the targeting ligand of a nanoparticle-based drug delivery system. Vinorelbine (VRL) loaded PLGA-PEG nanoparticles (NP) were formulated...


Enhanced cytotoxicity of optimized liposomal genistein via specific induction of apoptosis in breast, ovarian and prostate carcinomas.

Abstract Clinical use of genistein against cancer is limited by its extremely low aqueous solubility, poor bioavailability and pharmacokinetics. Based on structural analogy with steroidal compounds, liposomal vehicle compositions were designed and optimized for maximum incorporation of genistein's flavonoid structure. Model conventional and stealth liposomes of genistein (GenLip) - incorporating unsaturated phospholipids and cholesterol - have demonstrated enhanced drug solubilization (over 350-folds > aque...


Effects of Tyroserleutide on phosphatidylinositol 3'-kinase/AKT pathway in human hepatocellular carcinoma cell.

Abstract Tyroserleutide (YSL) is an active, low-molecular-weight polypeptide with in vitro and in vivo anticancer effects on human hepatocellular carcinoma BEL-7402 cells. In this study, we studied the effects of YSL on PI3K/AKT in the BEL-7402 cells to explore its anti-tumor mechanism. Results showed that YSL could up-regulate the mRNA and protein expression of tumor suppressor PTEN and increase their activities, meanwhile inhibited the mRNA and protein expression of oncogene AKT and decreased the kinase a...


Chitosan-assisted immobilization of serratiopeptidase on magnetic nanoparticles, characterization and its target delivery.

Abstract Background: Magnetic nanoparticles (MNPs) gained attentions as universal carrier for drug delivery and for enzyme immobilization. Purpose: Target delivery of serratiopeptidase for treatment using this enzyme and applications in drug delivery. Method: Serratiopeptidase was immobilized on chitosan amino-functionalized MNPs by covalent bonding through glutaraldehyde. Targeting of MNPs with immobilized enzyme (EMNPs) was carried out in vitro in modified diffusion cell and in vivo in rats. Results and d...

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